Research progress from mainly over the last five years is described for a multidisciplinary collaborative program project directed toward the discovery of potential anticancer agents from a broad range of taxonomically defined organisms. Selected lead compounds with potential as new antitumor agents that are representative of considerable structural diversity have continued to be obtained from each of tropical plants, terrestrial and aquatic cyanobacteria, and filamentous fungi. Recently, a new focus has been on the investigation of the constituents of U.S. lichens and their fungal mycobionts. A medicinal chemistry and pharmacokinetics component of the project has optimized structurally selected lead natural products, leading to enhanced cytotoxic potencies against selected cancer cell lines. Biological testing has shown several compounds to have in vivo activity, and relevant preliminary structure-activity relationship and mechanism of action studies have been performed. Several promising lead compounds worthy of further investigation have been identified from the most recent collaborative work performed.

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Covering: 2006 to 2013. Investigations on the chemistry and biology of rocaglamide, silvestrol and structurally related bioactive compounds from Aglaia species during the period 2006-2013 are reviewed. Included are new phytochemical studies of naturally occurring rocaglamide derivatives, an update on synthetic methods for cyclopenta[b]benzofurans, and a description of the recent biological evaluation and mechanism-of-action studies on compounds of this type.

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Seven new cycloartanes, argenteanones C-E (4-6) and argenteanols B-E (7-10), have been isolated from Aglaia argentea leaves. All of these compounds possess significant cytotoxic activity against KB cells (IC50 values between 3.7 and 6.2 micrograms/mL). Structure elucidation was performed by 2D NMR spectroscopy, aided by molecular modeling in the case of the side chain of compound 7.

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Aglaia argentea leaves yielded three new cycloartanes: argenteanones A and B, and argenteanol. The first two possess cytotoxic activity against KB cells (IC50 7.5 micrograms ml-1 and 6.5 micrograms ml-1 respectively). Structural elucidation was done by two-dimensional NMR spectroscopy.

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